Glucuronidation of aurantio-obtusin: identification of human UDP-glucuronosyltransferases and species differences

Xenobiotica. 2014 Aug;44(8):716-21. doi: 10.3109/00498254.2014.895881. Epub 2014 Mar 11.

Abstract

1. The aurantio-obtusin's glucuronide was detected when aurantio-obtusin was incubated with human liver microsomes (HLMs). Recombinant UGT isoforms screening experiment showed that UGT1A8 was the major isoform contributed to the glucuronidation. 2. The metabolic profiles for aurantio-obtusin in liver microsomes from different species were similar, however, the intrinsic clearance values (Vmax/Km) among the species were: Monkey > Human > Rat > Rabbit > Dog > Pig > Mouse > Guinea pig.

Keywords: Aurantio-obtusin; UDP-glucuronosyltransferase (UGT); species difference.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthraquinones / metabolism*
  • Enzyme Assays
  • Glucuronides / chemistry
  • Glucuronides / metabolism*
  • Glucuronosyltransferase / metabolism*
  • Humans
  • Kinetics
  • Mass Spectrometry
  • Microsomes, Liver / metabolism
  • Recombinant Proteins / metabolism
  • Species Specificity

Substances

  • Anthraquinones
  • Glucuronides
  • Recombinant Proteins
  • aurantio-obtusin
  • Glucuronosyltransferase